Drug Delivery Technology (DDT) has achieved new heights during the last few years as an essential component of drug development. The delivery of drugs exclusively to the diseased site is the only plausible solution for increasing their efficacy and simultaneously reducing the toxic effects. Ever since the unraveling of human genome in the beginning of the present century and subsequent emergence of proteomics and genomics as new disciplines has given a new thrust to gene therapy which is aimed at treating the cause rather than the symptoms unlike the conventional small molecule drugs. The desired gene is transferred to the target cell through a vector so that the desired protein itself is expressed in the patient’s body. This approach is an appropriate remedy for the fast mutations occurring in pathogens. The vector is invariably a virus or may be a non-virus, therefore, the novel drug delivery systems are either via viral or non-viral modes. The non-viral delivery systems may be either synthetic vectors, drug loaded tumour cells (DLTCs) as vectors, folates (folic acid conjugates) or it may be by applying physical or chemical methods. All these approaches have been described in this paper giving the latest achievements of each. The prodrug concept has also been elaborated concisely.